Flashcards in PharmII_Exam2 Deck (105):
Which receptor does Diphenhydramine(benadryl) blocks?
It blocks H1 selectively
Name two drugs that can cause degranulation independent release of histamine?
What two H receptors act in the CNS and Cardiovascular system?
H1 and H2
What is the antihistamine effect in the CNS?
Stimulation (nervousness and restlessness)
What are the cardiovascular effects of histamine?
Decrease in blood pressure (H1 and H2)
Increase in heart rate (H2)
What are the bronchiole effect when antihistamine is present?
Bronchoconstriction (H1 receptors)
What are the GI effects of antihistamines?
H1 - intestinal contraction
H2 - Parietal cells secrete HCl
Describe the three parts in the wheal and flare response?
1. reddening of the area - vascular smooth muscle dilation
2. Edematous wheal - endothelium
3. Red irregular flare surrounding the wheal - axon reflex.
What is the hypersensitivity response?
2. Hypotension, tachycardia
3. Increase in capillary permeability
Give me an example of a popular physiologic antagonist?
What are the three ways to block histamine reaction?
1. Physiological antagonist
2. Competitive antagonists
3. Inhibit the release
What is a summary of the 1st generation H1 antagonists?
More autonomic receptor blockade.
Name the 4 categories of 1st generation antagonists?
2. Piperazine Derivatives
What is so special about Ethanolamines?
More Anti-muscarinic actions
Motion sickness blockage
What separates the Piperazine Derivatives from the other H1 antagonists?
They are longer acting.
What is so special about Alkylamines and Phenothiazines?
They are more potent
What separates the 2nd generation drugs from the first?
They are less sedating.
They do not cross the BBB as easily or not at all
What are the two category of drugs found in 2nd gen antagonists?
What is Allegra used for?
This is a 2nd generation H1 antagonists.
Does H1 1st gen or 2nd gen drugs last longer?
2nd gen drugs.
Which 2nd generation drug contains the most sedation out of the generation?
What conditions are antihistamines really good for?
What condition is antihistamine not good for?
Which generation do you give to ppl suffering from Allergic rhinitis and chronic Urticaria
What drug is the best for motion sickness?
Drugs like Dromazine and promethazine are used
Antihistamines are used in sleeps aids?
Sold OTC due to sedating effects.
What age does the child have to be to use anti-histamine?
What is the exception?
Over two years old.
Zyrtec can be used over 6 months.
Anti-histamines lead to seizures
Name the four topical agents for anti-histamines?
What percentage of headaches do tension headaches compose of?
How can primary headaches be classified as?
What drug do you use to treat gout?
Acetaminophen is a NSAID?
It has no anti-inflammatory properties
What are some adverse effects in NSAIDs?
Mild to moderate GI irritation
What are the three components found in prostanoids?
What occurs in phase I?
WBC bind to endothelial cells.
Become active, infiltrate
What occurs in phase 2?
WBC are activated for phagocytosis or lysosomal enzyme release
What occurs in phase 3?
Endothelial injury, tissue damage and inflammatory stimulus amp results.
Tell me about the enzyme COX 1?
It is constitutively expressed in all cells.
Housekeeping enzyme found in most cells
Tell me about COX2
It is an inducible enzyme.
You have to turn it on. Tissue damage will turn it on.
Tell me about COX-3
It is actually a splicing form of COX-1
It's function is unknown.
Prostanoid effect in the vascular system?
Thromboxane A2 = vasoconstriction
PGE2 and PGI2 = vasodilators
Prostanoid effect on GI?
Activate GI smooth muscle
Prostanoid effect on Airways?
PGs relax the airways
TXA2 and PGF2-alpha contracts
What happens if you block the COX1 mech in the GI?
You increase the amount of HCl that is released leading to ulcers.
Usually there is mucosal protection without this block.
What is the action of prostanoids in platelets?
PGE1 and PGEI2 inhibit the aggregation of platelets.
TXA2 stimulates the aggregation
What does a low dose of aspirin do in platelets?
It inhibits thromboxane A2 formation.
This is the cardioprotective effect
Loop diuretics will get reduced with the use of prostanoids?
Effects of prostanoids in the eye?
It lowers IOP
The effects of aspirin are reversible?
They are irreversible. Its effects are longer than that predicted by its 1/2 life.
The COX enzyme must be re-synthesized to return normal function.
Symptomatic relief is provided by NSAIDs in which of the three categories?
What percentage does NSAIDs reduce the chances of getting colon cancer?
Tell me about the relation COX-2 have with thrombotic events?
COX 2 does not mess with TXA2
COX2 does suppress PGI2
WHen u suppress PGI2, u lead to an activation of platelets and cause potential thrombotic events.
THe metabolism of aspirin is saturable?
ANother drug that is saturable is phenytoin
How long is a patient told not to take NSAIDs before surgery?
Because it takes 8-11 days for platelets to regenerate.
Which drug is Reye's syndrome linked to?
It is given to children with viral infections and fever.
Instead give the child acetaminophen or ibuprofen.
It is perfectly OK to use aspirin in gout?
Aspirin does not eliminate uric crystals
What are some adverse effects of aspirin intoxication?
Which drug is more potent than aspirin but not more efficacious?
What is so special about Clinoril?
Half as potent as Indocin.
Suppresses familial intestinal polyposis
INhibit the development of colon, breast, and prostate cancer.
Which drug is better tolerated than aspirin?
It is also just as efficacious.
It is indicated for use for rheumatic disease including the juvenile form
What drug can be used in place of opioids like morphine and is as efficacious for postoperative pain?
U can take ibuprofen while breastfeeding?
Which propionic acid has an increased Cardiovascular risk compared to a placebo with long term usage?
Which propionic acid derivative is the most potent?
Why do we use Cox2?
To prevent adverse GI effects and platelet actions
Which cylcooxygenase inhibitor class have a black box warning?
all NSAIDs that inhibit COX-2 (nonselective COx inhibitors and COX-2 selective agents),
except for aspirin - has cardioprotective features
Which two cox inhibitors were pulled from the market due to cardiovascular effects?
Acetaminophen has peripheral effects?
It does not inhibit peripheral COX enzymes. Does not inhibit platelet aggregation.
No severe GI problems.
What population is acetaminophen good in?
How do you treat toxicity from Acetaminophen?
Addition of sulfhydryl compounds to replenish glutathione.
What is the therapeutic approach to treat gout?
1. Reduce inflammation
2. Increase the elimination of Uric acid
3. Decrease the production of Uric acid
What is the function of colbenemid in gout?
Reduce the pain and inflammation.
MOA of colbenemd?
It binds to and blocks tubulin.
prevents its polymerization preventing leukocyte migration and phagocytosis of uric acid crystals.
which two classes of NSAIDs don't work in gout?
Salicylates and tolectin
Which NSAID is the best to use in gout?
Inhibits phagocytosis of urate crystals.
MOA of allopurinol?
Inhibits xanthine oxidase which Prevents uric acid biosynthesis
Analgesic efficacy is mediated via which receptor?
Which area in the brain contains a high concentration of
opioid receptors that facilitate feelings of euphoria.
Opioid withdrawal is life-threatening?
Alcohol and morphine is life threatening.
I should never give a patient an opioid due to its dependcence levels!
Despite the propensity for abuse and the development of dependence, these drugs should never be withheld as analgesics.
Which pain reacts well to opiates?
Stimulation of nociceptors along intact neural pathways.
Which pain does opiates react poorly to?
May need to increase the dose to have an effect.
Ascending pain pathway- Opioids inhibit the ascending pathway at the dorsal horn (spinal) and at the thalamus
Are the kappa receptors found in ascending or descending pathway?
They work oppositely form the mew receptor
Stimulation of descending pathway will do what?
Inhibit the ascending pathway.
When sensory input is high, is there more or less respiratory distress?
Ex: someone is injured; the sensory input is gonna be mad high. As the pain goes away, the sensory input will increase.
used for their ability to reduce acid secretions
Chronic postoperative pain or pain from inflammation is well-controlled by NSAIDs?
What does PGI2 do?
Normally suppresses platelet activation, so inhibiting it can cause
platelet over activation aka Thrombotic events. (this is why Vioxx and Bextra were withdrawn)
COX-2 selective agents and p-aminophenol derivatives are less harmful to the stomach because COX-1 is responsible for buffering stomach acid.
Secondary use for indocin?
closure of patent ductus arteriosis in premature babies
• Dental and cancer pain
• Better anti inflammatory than aspirin
• Used as an analgesic with less auditory, GI, and platelet side effects.
It is OK to use acetaminophen on any kind of gout?
Due to the fact that acetaminophen has no anti-inflammatory properties.
Which agents are better tolerated than aspirin and indomethacin
Efficacy is similar to the sals.
The sals are cheaper
Advantage is long 1/2 life so only single daily dose
Give me two examples of uricosuric agents?
How long do you wait after a gouty attack to start a patient on probenecid and sulfinpyrazone?
Wait 2-3 weeks.
U use these drugs when patient has had several acute attacks or if urate levels are very high and an attack is inevitable.
A new drug that is more effective at lowering serum ureate levels than allopurinol.
THere are hepatic problems causing death.
Name two examples of xanthine oxidase inhibitors?
Relatively high potency agent with selectivity for COX 2
Selective for COX 2.
Comparable efficacy with less GI effects.
Slightly selective for COX 2
Useful for post op pain.
What is an AE for etodolac?
Temporary renal problems.
Similar efficacy as other NSAIDs with fewer adverse GI effects
Pfizer has said that the prothrombotic effects seen with Vioxx don't happen at therapeutic doses of celebrex.